Abstract
A series of 2-aminomethyl piperidines has been discovered as novel urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent, cross-species active, and functional urotensin-II receptor antagonists such as 1a and 11a are described.
MeSH terms
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Binding Sites
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Humans
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Methylamines / chemical synthesis
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Methylamines / pharmacology*
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Models, Chemical
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Piperidines / chemical synthesis
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Piperidines / pharmacology*
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Receptors, G-Protein-Coupled / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Vasoconstrictor Agents / chemical synthesis
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Vasoconstrictor Agents / pharmacology*
Substances
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Methylamines
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Piperidines
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Receptors, G-Protein-Coupled
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UTS2R protein, human
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Vasoconstrictor Agents